Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors
Copyright policy )Synthesis, in vitro and in silico screening of ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetates as protein-tyrosine phosphatase 1B inhibitors
The ethyl 2-(6-substituted benzo[d]thiazol-2-ylamino)-2-oxoacetate derivatives (OX 1-9) were prepared using a one-step reaction. The in vitro inhibitory activity of the compounds against protein tyrosine phosphatase 1B (PTP-1B) was evaluated. Compounds OX-(1, 6 and 7) were rapid reversible (mixed-type) inhibitors of PTP-1B with IC(50) values in the low micro-molar range. The most active compounds OX-(1, 6 and 7) were docked into the crystal structure of PTP-1B. Docking results indicate potential hydrogen bond interactions between the oxamate group in all compounds and the catalytic amino acid residues Arg221 and Ser216. The compounds were evaluated for their in vivo hypoglycemic activity, showing significant lowering of plasma glucose concentration in acute normoglycemic model and oral glucose tolerance test similarly at the effect exerted for hypoglycemic drug glibenclamide.
Male, Models, Molecular, Protein Tyrosine Phosphatase, Non-Receptor Type 1, Protein Conformation, Drug Evaluation, Preclinical, Computational Biology, Chemistry Techniques, Synthetic, Glucose Tolerance Test, Rats, Diabetes; Protein tyrosine phosphatase; PTP-1B; Benzothiazole, Animals, Humans, Hypoglycemic Agents, Benzothiazoles, Enzyme Inhibitors, Rats, Wistar
Male, Models, Molecular, Protein Tyrosine Phosphatase, Non-Receptor Type 1, Protein Conformation, Drug Evaluation, Preclinical, Computational Biology, Chemistry Techniques, Synthetic, Glucose Tolerance Test, Rats, Diabetes; Protein tyrosine phosphatase; PTP-1B; Benzothiazole, Animals, Humans, Hypoglycemic Agents, Benzothiazoles, Enzyme Inhibitors, Rats, Wistar
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